CA2977415A1 - Tesofensine, beta blocker combination formulation - Google Patents
Tesofensine, beta blocker combination formulation Download PDFInfo
- Publication number
- CA2977415A1 CA2977415A1 CA2977415A CA2977415A CA2977415A1 CA 2977415 A1 CA2977415 A1 CA 2977415A1 CA 2977415 A CA2977415 A CA 2977415A CA 2977415 A CA2977415 A CA 2977415A CA 2977415 A1 CA2977415 A1 CA 2977415A1
- Authority
- CA
- Canada
- Prior art keywords
- composition
- beta blocker
- metoprolol
- tesofensine
- carvedilol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- Veterinary Medicine (AREA)
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DKPA201570117 | 2015-03-03 | ||
DKPA201570117 | 2015-03-03 | ||
DKPA201570644 | 2015-10-09 | ||
DKPA201570644 | 2015-10-09 | ||
PCT/DK2016/050058 WO2016138908A1 (en) | 2015-03-03 | 2016-03-02 | Tesofensine, beta blocker combination formulation |
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CA2977415A1 true CA2977415A1 (en) | 2016-09-09 |
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CA2977415A Pending CA2977415A1 (en) | 2015-03-03 | 2016-03-02 | Tesofensine, beta blocker combination formulation |
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EP (1) | EP3265126B1 (ru) |
JP (1) | JP6772430B2 (ru) |
KR (1) | KR101999463B1 (ru) |
CN (1) | CN107666913B (ru) |
AU (1) | AU2016228002B2 (ru) |
CA (1) | CA2977415A1 (ru) |
CL (1) | CL2017002214A1 (ru) |
CO (1) | CO2017009930A2 (ru) |
CR (1) | CR20170447A (ru) |
DK (1) | DK3265126T3 (ru) |
DO (1) | DOP2017000219A (ru) |
EA (1) | EA033298B1 (ru) |
EC (1) | ECSP17059323A (ru) |
ES (1) | ES2885437T3 (ru) |
GT (1) | GT201700194A (ru) |
HK (1) | HK1247127A1 (ru) |
HR (1) | HRP20211361T1 (ru) |
HU (1) | HUE055974T2 (ru) |
IL (1) | IL254179B (ru) |
LT (1) | LT3265126T (ru) |
MA (1) | MA41634B1 (ru) |
MX (1) | MX2017011257A (ru) |
PE (1) | PE20180187A1 (ru) |
PH (1) | PH12017501509A1 (ru) |
PL (1) | PL3265126T3 (ru) |
PT (1) | PT3265126T (ru) |
RS (1) | RS62275B1 (ru) |
SA (1) | SA517382209B1 (ru) |
SG (1) | SG11201706899VA (ru) |
SI (1) | SI3265126T1 (ru) |
UA (1) | UA122224C2 (ru) |
WO (1) | WO2016138908A1 (ru) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL2814473T3 (pl) * | 2012-02-16 | 2019-06-28 | Saniona A/S | Kompozycje farmaceutyczne do terapii skojarzonej |
PT3265126T (pt) | 2015-03-03 | 2021-08-30 | Saniona As | Formulação combinada de tesofensina e metoprolol |
EP3402473A1 (en) * | 2016-01-15 | 2018-11-21 | Saniona A/S | Tesofensine and metoprolol for treatment of hypertension |
JP6612004B1 (ja) * | 2018-07-31 | 2019-11-27 | 株式会社親広産業 | グルコース消費促進剤および解糖系促進剤 |
WO2020026471A1 (ja) * | 2018-07-31 | 2020-02-06 | 株式会社親広産業 | グルコース消費促進剤および解糖系促進剤 |
MX2021008208A (es) * | 2019-01-07 | 2021-11-17 | Saniona As | Tesofensina para la reduccion del peso corporal para pacientes con sindrome de prader-willi. |
JP2023523738A (ja) | 2020-04-22 | 2023-06-07 | サニオナ エー/エス | 視床下部性肥満症の処置 |
CN117045610B (zh) * | 2023-08-24 | 2024-04-30 | 杭州沐源生物医药科技有限公司 | 一种溶出高稳定性的盐酸拉贝洛尔组合物及其制备方法 |
Family Cites Families (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1992016197A1 (en) | 1991-03-18 | 1992-10-01 | Sepracor Inc. | Composition and method containing optically pure (s) metoprolol |
PT885220E (pt) | 1996-02-22 | 2001-11-30 | Neurosearch As | Derivados de tropano a sua preparacao e utilizacao |
US5885616A (en) * | 1997-08-18 | 1999-03-23 | Impax Pharmaceuticals, Inc. | Sustained release drug delivery system suitable for oral administration |
US6638937B2 (en) | 1998-07-06 | 2003-10-28 | Bristol-Myers Squibb Co. | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists |
SE0100200D0 (sv) * | 2001-01-24 | 2001-01-24 | Astrazeneca Ab | New film coating |
DE10129725A1 (de) | 2001-06-20 | 2003-01-02 | Bayer Ag | Kombinationstherapie substituierter Oxazolidinone |
US8101209B2 (en) | 2001-10-09 | 2012-01-24 | Flamel Technologies | Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles |
HUP0200849A2 (hu) | 2002-03-06 | 2004-08-30 | Sanofi-Synthelabo | N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra |
AU2003282375A1 (en) | 2003-02-05 | 2004-08-30 | Ipca Laboratories Limited | Pharmaceutical compositions and process of production thereof |
AU2004234158B2 (en) | 2003-04-29 | 2010-01-28 | Pfizer Inc. | 5,7-diaminopyrazolo[4,3-D]pyrimidines useful in the treatment of hypertension |
US7314640B2 (en) * | 2003-07-11 | 2008-01-01 | Mongkol Sriwongjanya | Formulation and process for drug loaded cores |
WO2005070427A1 (en) | 2004-01-22 | 2005-08-04 | Neurosearch A/S | Compounds for the sustained reduction of body weight |
DE102005034351A1 (de) | 2005-07-22 | 2007-01-25 | Sension, Biologische Detektions- Und Schnelltestsysteme Gmbh | Farb-Umschlag-Indikator zur Statusanzeige von RFID-Tickets und -Etiketten |
US20070053983A1 (en) | 2005-09-06 | 2007-03-08 | Girish Jain | Extended release compositions of metoprolol succinate |
US20070092573A1 (en) | 2005-10-24 | 2007-04-26 | Laxminarayan Joshi | Stabilized extended release pharmaceutical compositions comprising a beta-adrenoreceptor antagonist |
DE602006018529D1 (de) | 2005-12-29 | 2011-01-05 | Osmotica Kereskedelmi Es Szolgaltato Kft | Mehrschichtige tablette mit dreifacher freisetzungskombination |
US20090068260A1 (en) * | 2006-02-24 | 2009-03-12 | Tomer Gold | Beta-1-selective adrenoceptor blocking agent compositions and methods for their preparation |
US20070202172A1 (en) * | 2006-02-24 | 2007-08-30 | Tomer Gold | Metoprolol succinate E.R. tablets and methods for their preparation |
US8815285B2 (en) | 2006-03-28 | 2014-08-26 | Wockhardt Ltd. | Extended release dosage forms of metoprolol |
DE102006020604A1 (de) | 2006-05-02 | 2007-11-08 | Bayer Healthcare Ag | Flüssige Arzneimittelformulierung |
CA2657202A1 (en) | 2006-07-28 | 2008-01-31 | Farmaprojects, S.A. | Extended release pharmaceutical formulation of metoprolol and process for its preparation |
EP2222302A1 (en) | 2007-11-20 | 2010-09-01 | NeuroSearch A/S | A method for treating over-eating disorders |
WO2009080691A2 (en) | 2007-12-20 | 2009-07-02 | Neurosearch A/S | Pharmaceutical composition comprising tesofensine or its analogue and an anti-obesity compound |
WO2009080693A2 (en) * | 2007-12-20 | 2009-07-02 | Neurosearch A/S | Pharmaceutical composition comprising tesofensine or its analogue and a beta blocker |
RU2010131022A (ru) | 2007-12-27 | 2012-02-10 | Байер Энимэл Хельс ГмбХ (DE) | ЛЕЧЕНИЕ ЗАБОЛЕВАНИЯ СЕРДЦА С ПРИМЕНЕНИЕМ β-БЛОКАТОРОВ |
US9408837B2 (en) | 2008-05-28 | 2016-08-09 | Kitov Pharmaceutical Ltd. | Ameliorating drug-induced elevations in blood pressure by adjunctive use of antihypertensive drugs |
EP2406253B1 (en) | 2009-03-11 | 2013-07-03 | Pfizer Inc. | Benzofuranyl derivatives used as glucokinase inhibitors |
AU2010255422B2 (en) | 2009-06-05 | 2014-04-10 | Pfizer Inc. | 1- ( piperidin-4-yl) -pyrazole derivatives as GPR 119 modulators |
JP5827952B2 (ja) * | 2009-10-09 | 2015-12-02 | ユンジン・ファーム・カンパニー・リミテッドYungjin Pharm. Co. Ltd. | 速効性と持続性を同時に有する薬剤学的組成物 |
JP5696156B2 (ja) | 2009-11-02 | 2015-04-08 | ファイザー・インク | ジオキサ−ビシクロ[3.2.1]オクタン−2,3,4−トリオール誘導体 |
US10485770B2 (en) | 2009-12-21 | 2019-11-26 | Aptapharma, Inc. | Functionally-coated multilayer tablets |
CN102145000A (zh) * | 2010-02-06 | 2011-08-10 | 赤峰维康生化制药有限公司 | 一种坎地沙坦酯和美托洛尔复方制剂 |
CN102198112A (zh) * | 2010-03-26 | 2011-09-28 | 北京天衡药物研究院 | 一种渗透泵型控释片及其制备方法 |
US8235632B2 (en) | 2010-05-14 | 2012-08-07 | Illinois Tool Works Inc. | Cargo bag valve deflector |
WO2011144975A1 (en) * | 2010-05-15 | 2011-11-24 | Jubilant Life Sciences Limited | Multi-unit compositions |
WO2012052834A2 (en) | 2010-10-21 | 2012-04-26 | Inventia Healthcare Private Limited | Multiple unit particulate system comprising metoprolol succinate |
CN102085195A (zh) * | 2011-01-10 | 2011-06-08 | 中国药科大学 | 琥珀酸美托洛尔缓释片及其制备方法 |
SG194605A1 (en) | 2011-05-06 | 2013-12-30 | Glaxosmithkline Llc | Sustained release paracetamol formulations |
WO2013001516A1 (en) * | 2011-06-29 | 2013-01-03 | Ranbaxy Laboratories Limited | Multilayered dosage form |
CN103906508A (zh) | 2011-08-26 | 2014-07-02 | 沃克哈特有限公司 | 治疗心血管疾病的方法 |
RU2014127884A (ru) | 2011-12-09 | 2016-02-10 | Вокхардт Лимитед | Способы лечения сердечно-сосудистого нарушения |
PL2814473T3 (pl) | 2012-02-16 | 2019-06-28 | Saniona A/S | Kompozycje farmaceutyczne do terapii skojarzonej |
IN2012DE00826A (ru) | 2012-03-21 | 2015-08-21 | Ranbaxy Lab Ltd | |
CN102626396B (zh) * | 2012-04-28 | 2014-05-07 | 海南华益泰康药业有限公司 | 一种美托洛尔缓释片剂及其制备方法 |
EP3019160A1 (en) | 2013-07-09 | 2016-05-18 | Sun Pharmaceutical Industries Ltd | Extended-release pharmaceutical compositions of metoprolol |
PT3265126T (pt) | 2015-03-03 | 2021-08-30 | Saniona As | Formulação combinada de tesofensina e metoprolol |
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